N-[[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]-thioxomethyl and carbonyl]-N-methylglycinamides

Abstract

Disclosed herein are tolrestat and oxotolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

We claim: 
     
       1. A compound of formula I ##STR12## wherein R is selected from the group consisting of --NH 2 , --NHCH 3 , --N(CH 3 ) 2 , ##STR13## and X is oxygen and the pharmaceutically acceptable salts thereof. 
     
     
       2. The compound of claim 1 which is N-[[6-methoxy-5-trifluoromethyl)-1-naphthalenyl]carbonyl]-N-methylglycinamide. 
     
     
       3. A pharmaceutical composition for preventing or relieving neuropathy in a diabetic mammal, which comprises an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier. 
     
     
       4. A method of preventing or relieving neuropathy in a diabetic mammal, which comprises administering to said mammal an alleviating or prophylactic amount of a compound of claim 1. 
     
     
       5. A method of preventing or relieving nephtopathy in a diabetic mammal, which comprises administering to said mammal an alleviating or prophylactic amount of a compound of claim 1. 
     
     
       6. A method of preventing or relieving retinopathy in a diabetic mammal, which comprises administering to said mammal an alleviating or prophylactic amount of a compound of claim 1. 
     
     
       7. A method of preventing or relieving cataracts in a diabetic mammal, which comprises administering to said mammal an alleviating or prophylactic amount of a compound of claim 1.